Quinolones have been shown to be effective to varying degrees against a range of certain anaerobic pathogens. However, as diseases caused by these pathogens are on the rise, there exists a need for antimicrobial compounds that are more potent than the present group of quinolones.
Gemifloxacin mesylate (SB-265805) is a novel fluoroquinolone useful as a potent antibacterial agent. Gemifloxacin compounds are described in detail in patent application PCT/KR98/00051 published as WO 98/42705. Patent application EP 688772 discloses novel quinoline(naphthyridine)carboxylic acid derivatives, including anhydrous (R,S)-7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluo ro-4-oxo-1,4-dihydro-8-naphthyridine-3-carboxylic acid of formula I. ##STR1##
PCT/KR98/00051 discloses (R,S)-7-(3-aminomethyl-4-syn-methoxyimino-pyrrolidin-1-yl)-1-cyclopropyl-6 -fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof including the sesquihydrate.
While in vitro testing of new antimicrobial compounds is often extensive, these studies tend to focus on a limited range of typical anaerobic bacterial pathogens (Cormicon, et al., Antimicrob. Agents Chemother., 41:204-211, 1997; Hohl, et al., Clin. Microbiol. Infect., 4:280-284, 1998; Marco, et al., J. Antimicrob. Chemother., 40:605-607, 1997). Moreover, it has been reported that (Goldstein, et al., Antimicrob. Agents Chemother., Submitted) the activity of gemifloxacin against typical anaerobic bacteria; it showed activity against Bacteroides fragilis and certain Prevotella and Porphyromonas strains, but only limited activity against B. thetaiotaomicron, B. distasonis and B. ovatus. Data is lacking about the activities of new quinolone compounds against many of the less frequently encountered anaerobic pathogens, such as Actinomyces spp., Anaerobiospirrilum spp., Porphyromonas spp., and Bilophila wadsworthia.
Provided herein is an invention based, in part, on a significant discovery made using a gemifloxacin compound against various unusual, though medically impotant, anaerobic bacteria, demonstrating the activity of the gemifloxacin compound used was superior to a number of quinolones as described in more detail herein. Gemifloxacin compounds are valuable compounds for the treatment of bacterial caused by a range of anaerobic pathogens, including those resistant to usual oral therapy, thereby filling an unmet medical need.